沃替西汀有关物质的合成  

Synthesis of Related Substances of Vortioxetine

作　　者：周成凯 姜开元 岳慧 方浩[3] 隋强 ZHOU Chengkai;JIANG Kaiyuan;YUE Hui;FANG Hao;SUI Qiang(School of Chemistry and Chemical Engineering,Shanghai University of Engineering Science,Shanghai 201620;China State Institute of Pharmaceutical Industry,Shanghai 201203;Shandong University,Jinan 250012)

机构地区：[1]上海工程技术大学化学化工学院,上海201620 [2]中国医药工业研究总院,上海201203 [3]山东大学,山东济南250012

出　　处：《中国医药工业杂志》2021年第7期895-900,共6页Chinese Journal of Pharmaceuticals

摘　　要：为控制沃替西汀的质量,本研究基于其合成工艺,制备了在药物中发现的5个有关物质,分别为1-[2-[(5-氯-2,4-二甲基苯基)硫基]苯基]哌嗪氢溴酸盐(A-HBr)、1-苯基-4-[2-[(2,4-二甲基苯基)硫基]苯基]哌嗪(B)、1,2-双[(2,4-二甲苯基)硫基]苯(C)、[1,1'-二萘]-2,2'-二基双(二苯基氧化膦)(D)、2-二苯基膦基-2'-二苯基氧膦基-1,1'-联萘(E)。其中,有关物质B和有关物质E是本文首次报道。上述有关物质的结构均经^(1)H NMR、MS和元素分析确证。In order to control the quality of vortioxetine,five related substances found in API,namely 1-[2-[(5-chloro-2,4-dimethylphenyl)thio]phenyl]piperazine hydrobromide(A-HBr),1-phenyl-4-[2-[(2,4-dimethylphenyl)thio]piperazine(B),1,2-bis[(2,4-dimethylphenyl)thio]benzene(C),1,1'-(1,1'-Binaphthalene)-2,2'-diylbis(1,1-diphenylphosphine oxide)(D)and 2-diphenylphosphino-2'-diphenylphosphino-1,1'-binaphthyl(E),were synthesized based on the synthetic process of API.Among them,both related substance B and E have not found in the literatures.The structures of the above five compounds were confirmed by ^(1)H NMR,MS and elemental analysis.

关 键 词：沃替西汀 有关物质 结构确证 

分 类 号：R914[医药卫生—药物化学]